U.S. Pat. No. 6,127,357 discloses compounds of the general formula (I):
and pharmaceutically acceptable acid addition salts thereof wherein:A is alkylene chain of 2 to 4 carbon atoms optionally substituted by one or more lower alkyl groups,Z is oxygen or sulfur,R is H or lower alkyl,R1 is a mono or bicyclic aryl or heteroaryl radical,R2 is a mono or bicyclic heteroaryl radical, andR3 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkyl(lower)alkyl, aryl, aryl(lower)alkyl, heteroaryl, heteroaryl(lower)alkyl, a group of formula —NR4R5 [where R4 is hydrogen, lower alkyl, aryl or aryl(lower)alkyl and R5 is hydrogen, lower alkyl, —CO(lower)alkyl, aryl, -Coaryl, aryl(lower)alkyl, cycloalkyl, or cycloalkyl-(lower)alkyl or R4 and R5 together with the nitrogen atom to which they are both attached represent a saturated hetrocyclic ring which may contain a further heteroatom], or a group of formula OR6 [where R6 is lower alkyl, cycloalkyl, cycloalkyl(lower)alkyl, aryl, aryl (lower)alkyl, heteroaryl or heteroaryl(lower)alkyl].
WO 97/03982 discloses compounds of the general formula (II):
including enantiomers and the pharmaceutically acceptable acid addition salts thereof.
The compounds of formula (II) fall within the disclosure of U.S. Pat. No. 6,127,357 but are not specifically disclosed therein Compounds of Formula II were taught to have potent 5-HT1A antagonist activity in vivo when administered by the oral route.